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Excitatory Amino Acids - Clinical Results with Antagonists
Paul L. Herrling (Ed.)
Verlag Elsevier Trade Monographs, 1997
ISBN 9780080531342 , 156 Seiten
Format PDF
Kopierschutz DRM
Geräte
Front Cover
1
Excitatory Amino Acids – Clinical Results with Antagonists
4
Copyright Page
5
Contents
6
Contributors
10
Preface
12
Acknowledgments
14
Chapter 1. Selfotel (CGS 19755)
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1. Summary
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2. Overview of the pharmacology
17
3. Rationale for clinical testing
19
4. Human results
19
5. Conclusions
21
Chapter 2. D-CPPene (SDZ EAA-494)—A Competitive NMDA Antagonist: Pharmacology and Results in Humans
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1. Summary
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2. Structure-activity relationships
23
3. General pharmacology
26
4. Human studies
32
5. Discussion
35
6. Conclusion
36
Chapter 3. Intrathecal Administration of a Competitive NMDA Receptor Antagonist for Pain Treatment
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1. Summary
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2. Overview of the pharmacology
38
3. Rationale for clinical testing
39
4. Human results
40
5. Discussion
41
Chapter 4. Clinical Experience with the NMDA Ion Channel Blocker, Aptiganel Hydrochloride (CERESTAT®)
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1. Summary
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2. Pharmacology
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3. Clinical studies in normal male volunteers
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4. Clinical studies in patients
49
5. Discussion
56
Chapter 5. Development of ACPC, A Partial Agonist of the Glycine Site on the NMDA Receptor
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1. Introduction
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2. Partial agonism as a therapeutic approach
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3. ACPC – pharmacology and mechanism of action
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4. Efficacy of ACPC in animal models of neuroprotection
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5. Efficacy of ACPC in animal models of depression and anxiety
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6. Prevention of opiate tolerance and toxicity by ACPC
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7. Pharmacokinetics
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8. Safety profiles of ACPC in animal models
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9. PCP-like effects
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10. Phase I clinical trials of ACPC
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Chapter 6. Ifenprodil and Eliprodil: Neuroprotective NMDA Receptor Antagonists and Calcium Channel Blockers
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1. Introduction
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2. The NMDA receptor complex and its regulation
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3. Actions of ifenprodil and eliprodil at different sites of the NMDA receptor
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4. Other sites of action of ifenprodil and eliprodil
86
5. Neuroprotective effects
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6. Behavioral pharmacology and side-effect profile
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7. Pharmacokinetics
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8. Clinical trials
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9. Conclusions
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Chapter 7. (3S,4aR,6R,8aR)-6-[2-(1(2)H-Tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic Acid (LY293558) and its Racemate (LY215490): A Selective and Competitive AMPA/Kainate Receptor Antagonist
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1. Summary
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2. LY293558 as a novel neuroprotectant compound
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3. In vitro glutamate receptor profile
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4. In vivo AMPA receptor antagonism
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5. Effects of LY293558 on CNS excitability
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6. In vivo neuroprotection against AMPA-induced excitotoxicity
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7. Neuroprotectant activity in animal models of cerebral ischemia
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8. Overview and discussion
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Chapter 8. The NBQX Story
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1. Summary
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2. Pharmacology
104
3. Human pharmacology
111
4. Discussion
112
Chapter 9. Riluzole in Amyotrophic Lateral Sclerosis
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1. Summary
114
2. Introduction
114
3. Chemical structure
115
4. Neuroprotective properties
115
5. Mechanism(s) of action
116
6. Rationale of clinical testing
116
7. Clinical results
117
8. Conclusion
123
Chapter 10. Preclinical and Clinical Aspects of Remacemide Hydrochloride
124
1. Preclinical efficacy studies
124
2. Clinical studies
132
3. Conclusions
135
Glossary
136
Summary Table of Compounds and Their Clinical Status
140
References
144
Index
168
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